Stable self-emulsifying solid composition containing ivermectin medicine

Abstract

The invention aims to solve the technical problem so as to improve the water solubility of the ivermectin medicine and overcomes the defect that the ivermectin medicine is easy to hydrolyze under an acidic condition, so that the aims of improving the release rate of the medicine in a human body and preventing the medicine from being damaged or less damaged in an acidic gastric fluid are achieved;secondly, the problems of acid / alkali catalytic degradation and oxydative degradation of active ingredients during the preservation of the medicine are solved, so that effective components of the medicine are less degraded. The optimized composition provided by the invention contains the ivermectin medicine, a polyoxyethylene hydrogenated castor oil condensation compound, Arabic gum or / and polyvinylpyrrolidone, benzyl benzoate or azone, 1,2-propylene glycol and corncob powder; the composition can be also added with other anti-parasitic medicine, and optimally, the other anti-parasitic medicineis cyromazine.

Description

technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and in particular relates to a preparation technology of a pharmaceutical composition containing ivermectin. The composition prepared by the technology has the characteristics of high drug dissolution rate and more resistance to acid / alkali catalyzed degradation. Background technique [0002] Tests and data records: (1) Ivermectins are almost insoluble in water. For example, only 6-9 micrograms of ivermectin can be dissolved in 1 liter of water. Therefore, when preparing oral solid preparations containing ivermectin drugs, in order to ensure that the drugs can be absorbed more, improving the water solubility of the drugs is a technical link that must be considered. (2) There are two glycosidic bonds in the molecular structure of ivermectins, which are easily hydrolyzed by acid to lose sugar residues. For example, ivermectin is easily converted into the less active mo...

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Problems solved by technology

(3) The C2 position in the molecular structure of ivermectins is prone to epimerization under alkaline conditions and is converted into 2-epimer H 2 B 1a (2-epimer H 2 B 1a ), its anthelmintic activity is only H 2 B 1a About 1% of the activity; the double bond at the C3=C4 position is prone to shift and converts to a very low activity Δ 2，3 h 2 B 1a (See Table 3); The lactone bond that has in the molecular structure of ivermectin is also easy to be by OH - attacked and destroyed

(4) Ivermectin drugs are prone to oxidative degradation when in contact with air. When preparing solid preparations containing ivermectin drugs, it is difficult to meet expectations by adding antioxidants to the preparation to solve the problem of oxidative degradation of drugs. Effect

However, if the surfactant is not selected properly, it will make the drug more susceptible to acid / base catalyzed degradation

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